WO2005115365A2 - Pharmaceutical or cosmetic composition comprising mequinol and at least one depigmenting agent - Google Patents

Pharmaceutical or cosmetic composition comprising mequinol and at least one depigmenting agent Download PDF

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Publication number
WO2005115365A2
WO2005115365A2 PCT/FR2005/001211 FR2005001211W WO2005115365A2 WO 2005115365 A2 WO2005115365 A2 WO 2005115365A2 FR 2005001211 W FR2005001211 W FR 2005001211W WO 2005115365 A2 WO2005115365 A2 WO 2005115365A2
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WO
WIPO (PCT)
Prior art keywords
composition
depigmenting
mequinol
skin
depigmenting agent
Prior art date
Application number
PCT/FR2005/001211
Other languages
French (fr)
Other versions
WO2005115365A3 (en
Inventor
Isabelle Pelisson
André Jomard
Cécile COUSIN
Original Assignee
Galderma Research & Development, S.N.C.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Galderma Research & Development, S.N.C. filed Critical Galderma Research & Development, S.N.C.
Priority to EP05771145A priority Critical patent/EP1755541A2/en
Priority to JP2007512291A priority patent/JP2007537216A/en
Priority to CA002564104A priority patent/CA2564104A1/en
Priority to US11/596,356 priority patent/US20080159969A1/en
Publication of WO2005115365A2 publication Critical patent/WO2005115365A2/en
Publication of WO2005115365A3 publication Critical patent/WO2005115365A3/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42Amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

Definitions

  • the present invention relates to a new cosmetic or dermatological composition
  • a new cosmetic or dermatological composition comprising in combination mequinol (or 4-hydroxyanisole) and a depigmenting agent usable by topical application for depigmentation of the skin.
  • the composition according to the invention may also contain a sunscreen.
  • the pigmentation of the skin results from the synthesis of melanin in the melanocytes of the dermis by the transformation of tyrosine under the influence of a cuproprotein enzyme tyrosinase.
  • Mequinol or 4-hydroxyanisole has long been known as a compound having depigmenting activity (Brun R, Journal of the society of cosmetic chemists (1960), 11, 571-9).
  • mequinol as a depigmenting agent is to act as a substrate for tyrosinase (Riley P, Journal of Pathology (1969), 97 (2) 1 185-91 and Journal of Pathology (1969), 97 ( 2), 193-206.
  • Vitamin C or its derivatives are usually used as antioxidants at concentrations lower than 0.005% of the entire composition, as illustrated in US patent 6,353,029.
  • Kojic acid is already known in the prior art as a fungal metabolic with antioxidant properties, which causes contact dermatitis when its use is prolonged.
  • Azelaic acid has been reported in the literature as effective in the treatment of melasma, but this activity seems controversial (Sarkar et al., Dermatology 2002, 205: 249-254).
  • the invention therefore relates to a depigmenting composition for the skin comprising, in a physiologically acceptable medium, mequinol and at least one depigmenting agent chosen from the list consisting of kojic acid and its derivatives; azelaic acid and its derivatives; dicarboxylic acids; vitamin C and its derivatives, arbutin and its derivatives and paracetamol.
  • the depigmenting composition of the skin may comprise, as depigmenting agent kojic acid, azelaic acid or arbutin.
  • physiologically acceptable medium means a medium compatible with the skin, the mucous membranes and / or the integuments.
  • depigmenting agent means any active agent having a depigmenting activity on the skin. This activity makes it possible to decrease the already existing pigmentation of the skin and also to prevent any additional pigmentation greater than natural pigmentation.
  • composition comprising the combination according to the invention makes it possible to obtain a clear whitening of the skin.
  • the invention also relates to a depigmenting composition for the skin comprising, in a physiologically acceptable medium, mequinol, at least one depigmenting agent and at least one sunscreen.
  • the composition according to the invention advantageously comprises between 0.0001 and 20% by weight of mequinol relative to the total weight of the composition and between 0.025 and 20% by weight of depigmenting agent relative to the total weight of the composition, and preferably, respectively, between 0.001 and 10% by weight of mequinol relative to the total weight of the composition and between 0.05 and 10% by weight of depigmenting agent relative to the total weight of the composition.
  • the composition can also comprise at least one sunscreen in preferential concentrations ranging from 0.001 to 30.00% by weight relative to the total weight of the composition.
  • sun filters non-limiting examples that may be mentioned include physical sun filters such as titanium dioxide, zinc oxide and chemical sun filters such as octocrylene, ethylhexyl methoxycinnamate, octyl salicylate, avobenzone, oxybenzone, ecamsule or drometrizole trisiloxane, or mixtures thereof.
  • physical sun filters such as titanium dioxide, zinc oxide
  • chemical sun filters such as octocrylene, ethylhexyl methoxycinnamate, octyl salicylate, avobenzone, oxybenzone, ecamsule or drometrizole trisiloxane, or mixtures thereof.
  • the composition may include several sun filters.
  • each sunscreen can be added at a concentration ranging from 0.001 to 20% by weight relative to the total weight of the composition.
  • compositions according to the invention may also comprise any additive usually used in the cosmetic or pharmaceutical field, such as sequestrants, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids usual, mineral or organic, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, soothing and protective agents for the skin.
  • any additive usually used in the cosmetic or pharmaceutical field such as sequestrants, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids usual, mineral or organic, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, soothing and protective agents for the skin.
  • any additive usually used in the cosmetic or pharmaceutical field such as sequestrants, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids usual, mineral or organic, perfume
  • additives can be present in the composition in an amount of 0.001 to 20% by weight relative to the total weight of the composition.
  • the present invention also relates to a pharmaceutical composition as described above as a medicament.
  • the present invention also relates to a cosmetic composition.
  • compositions containing the combination according to the invention can have all the dosage forms normally used for topical application, for example in the form of solutions, gels, dispersions of the lotion or serum type, emulsions of liquid or semi-liquid consistency of the milk type, obtained by dispersion of a fatty phase in an aqueous phase (O / W) or vice versa (W / O), or of suspensions or emulsions of soft, semi-solid or solid consistency of cream or gel type, or else microemulsions, microcapsules, microparticles or vesicular dispersions of ionic and / or nonionic type.
  • These compositions are prepared according to the usual methods.
  • the cosmetic or dermatological compositions of the invention may contain adjuvants customary in the cosmetic or dermatological field, such as emulsifiers, hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents other than titanium oxide and ⁇ -hydroxy acid, preservatives, antioxidants, perfumes, fillers, filters and coloring matters.
  • adjuvants customary in the cosmetic or dermatological field, such as emulsifiers, hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents other than titanium oxide and ⁇ -hydroxy acid, preservatives, antioxidants, perfumes, fillers, filters and coloring matters.
  • the amounts of these various adjuvants are those conventionally used in the cosmetic and / or dermatological fields, and for example from 0.01% to 20% of the total weight of the composition.
  • These adjuvants depending on their nature, can be introduced into the fatty phase, into the aqueous phase and / or into the lipid vesicles.
  • the invention also relates to the use of the composition according to the invention as described above in the pharmaceutical and cosmetic field.
  • compositions of the invention are particularly suitable for the treatment and prevention of pigmentation disorders.
  • the compositions of the invention are suitable for the treatment and prevention of hyperpigmentary disorders such as melasma, chloasma, lentigines, senile lentigo, vitiligo, freckles, post-inflammatory hyperpigmentations due to abrasion. , a burn, a scar, a dermatosis, a contact allergy; nevi, hyperpigmentations with genetic determinism, hyperpigmentations of metabolic or drug origin, melanomas or any other hyperpigmentary lesions in particular those induced by photo induced or chronological aging of the skin and integuments.
  • compositions according to the invention are suitable for the treatment of melasma.
  • the compositions according to the invention also find an application in the cosmetic field, in particular in protection against the harmful aspects of the sun, in particular against pigmentary spots.
  • the invention also relates to a non-therapeutic cosmetic treatment process for beautifying the skin and / or improving its surface appearance, characterized in that a composition is applied to the skin and / or its integuments comprising mequinol and at least one depigmenting agent.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Toxicology (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention relates to a pharmaceutical or cosmetic composition comprising mequinol and at least one depigmenting agent in a physiologically acceptable medium. The invention also relates to the use thereof.

Description

COMPOSITION PHARMACEUTIQUE OU COSMETIQUE COMPRENANT DU MEQUINOL ET AU MOINS UN AGENT DEPIGMENTANT PHARMACEUTICAL OR COSMETIC COMPOSITION COMPRISING MEQUINOL AND AT LEAST ONE DEPIGMENTANT AGENT
La présente invention concerne une nouvelle composition cosmétique ou dermatologique comprenant en association le mequinol (ou 4-hydroxyanisole) et un dépigmentant utilisable par application topique pour la dépigmentation de la peau. La composition selon l'invention peut également contenir un filtre solaire.The present invention relates to a new cosmetic or dermatological composition comprising in combination mequinol (or 4-hydroxyanisole) and a depigmenting agent usable by topical application for depigmentation of the skin. The composition according to the invention may also contain a sunscreen.
La pigmentation de la peau résulte de la synthèse de la mélanine dans les mélanocytes du derme par la transformation de la tyrosine sous l'influence d'une enzyme cupro- protéique la tyrosinase.The pigmentation of the skin results from the synthesis of melanin in the melanocytes of the dermis by the transformation of tyrosine under the influence of a cuproprotein enzyme tyrosinase.
On peut donc obtenir un effet de dépigmentation de la peau en utilisant un composé qui dégrade la mélanine ou un inhibiteur de la tyrosinase qui bloque le mécanisme de transformation de la tyrosine en mélanine.We can therefore obtain a depigmentation effect on the skin by using a compound which degrades melanin or a tyrosinase inhibitor which blocks the mechanism of transformation of tyrosine into melanin.
Le mequinol ou 4-hydroxyanisole est connu de longue date comme étant un composé ayant une activité dépigmentant (Brun R, Journal of the society of cosmetic chemists (1960), 11 , 571-9).Mequinol or 4-hydroxyanisole has long been known as a compound having depigmenting activity (Brun R, Journal of the society of cosmetic chemists (1960), 11, 571-9).
Le mode d'action du mequinol en tant que dépigmentant est d'agir comme un substrat de la tyrosinase (Riley P, Journal of Pathology (1969), 97(2)1 185-91 et Journal of Pathology (1969), 97(2), 193-206.The mode of action of mequinol as a depigmenting agent is to act as a substrate for tyrosinase (Riley P, Journal of Pathology (1969), 97 (2) 1 185-91 and Journal of Pathology (1969), 97 ( 2), 193-206.
La vitamine C ou ses dérivés sont habituellement utilisés comme agents antioxydants à des concentrations inférieures à 0.005% de la totalité de la composition, comme illustré dans le brevet US 6,353,029.Vitamin C or its derivatives are usually used as antioxidants at concentrations lower than 0.005% of the entire composition, as illustrated in US patent 6,353,029.
L'acide kojique est déjà connu dans l'art antérieur comme un métabolique fongique ayant des propriétés antioxydantes, et qui provoque des dermatites de contact lorsque que son utilisation est prolongée.Kojic acid is already known in the prior art as a fungal metabolic with antioxidant properties, which causes contact dermatitis when its use is prolonged.
L'acide azélaïque a été rapporté dans la littérature comme efficace dans le traitement du mélasma mais cette activité semble controversée (Sarkar et al., Dermatology 2002, 205 :249-254).Azelaic acid has been reported in the literature as effective in the treatment of melasma, but this activity seems controversial (Sarkar et al., Dermatology 2002, 205: 249-254).
La Demanderesse a découvert de manière surprenante que la combinaison du mequinol et d'un agent dépigmentant pris dans une liste précise permettait par effet de synergie d'obtenir une réponse dépigmentante beaucoup plus efficace que celle obtenue avec le mequinol seul et ce avec des doses nettement plus faible.The Applicant has surprisingly discovered that the combination of mequinol and a depigmenting agent taken from a precise list makes it possible by synergistic effect to obtain a much more effective depigmenting response than that obtained with mequinol alone and this with significantly lower doses.
Ces quantités moindre permettront en outre de diminuer de manière significative les effets secondaires néfastes (rougeurs, irritations) liés à l'utilisation d'un dépigmentant.These lower amounts will also significantly reduce the harmful side effects (redness, irritation) associated with the use of a depigmenting agent.
L'invention se rapporte donc à une composition dépigmentante de la peau comprenant dans un milieu physiologiquement acceptable, du mequinol et au moins un agent dépigmentant choisi parmi la liste constituée par l'acide kojique et ses dérivés ; l'acide azélaique et ses dérivés ; les acides dicarboxyliques ; la vitamine C et ses dérivés, l'arbutine et ses dérivés et le paracétamol.The invention therefore relates to a depigmenting composition for the skin comprising, in a physiologically acceptable medium, mequinol and at least one depigmenting agent chosen from the list consisting of kojic acid and its derivatives; azelaic acid and its derivatives; dicarboxylic acids; vitamin C and its derivatives, arbutin and its derivatives and paracetamol.
En particulier, la composition dépigmentante de la peau pourra comprendre, comme agent dépigmentant l'acide kojique, l'acide azélaique ou l'arbutine.In particular, the depigmenting composition of the skin may comprise, as depigmenting agent kojic acid, azelaic acid or arbutin.
On entend par milieu physiologiquement acceptable, un milieu compatible avec la peau, les muqueuses et/ou les phanères.The term “physiologically acceptable medium” means a medium compatible with the skin, the mucous membranes and / or the integuments.
Par agent dépigmentant, on entend tout agent actif ayant une activité dépigmentante de la peau. Cette activité permet de diminuer la pigmentation déjà existante de la peau et également d'empêcher toute pigmentation supplémentaire supérieure à la pigmentation naturelle.The term “depigmenting agent” means any active agent having a depigmenting activity on the skin. This activity makes it possible to decrease the already existing pigmentation of the skin and also to prevent any additional pigmentation greater than natural pigmentation.
L'application d'une composition comprenant l'association selon l'invention permet d'obtenir un net blanchiment de la peau.The application of a composition comprising the combination according to the invention makes it possible to obtain a clear whitening of the skin.
L'invention se rapporte aussi à une composition dépigmentante de la peau comprenant dans un milieu physiologiquement acceptable, du mequinol, au moins un agent dépigmentant et au moins un filtre solaire.The invention also relates to a depigmenting composition for the skin comprising, in a physiologically acceptable medium, mequinol, at least one depigmenting agent and at least one sunscreen.
La composition selon l'invention comprend avantageusement entre 0,0001 et 20 % en poids de mequinol par rapport au poids total de la composition et entre 0.025 et 20 % en poids d'agent dépigmentant par rapport au poids total de la composition, et de préférence, respectivement, entre 0,001 et 10 % en poids de mequinol par rapport au poids total de la composition et entre 0,05 et 10 % en poids d'agent dépigmentant par rapport au poids total de la composition. La composition peut également comprendre au moins un filtre solaire dans des concentrations préférentielles allant de 0.001 à 30.00 % en poids par rapport au poids total de la composition. Parmi les filtres solaires, on peut citer à titre d'exemple non limitatif, les filtre solaires physiques tels que le dioxyde de titane, l'oxyde de zinc et les filtres solaires chimiques tels que l'octocrylene, l'ethylhexyl methoxycinnamate, l'octyl salicylate, l'avobenzone, l'oxybenzone, l'ecamsule ou le drometrizole trisiloxane, ou leurs mélanges.The composition according to the invention advantageously comprises between 0.0001 and 20% by weight of mequinol relative to the total weight of the composition and between 0.025 and 20% by weight of depigmenting agent relative to the total weight of the composition, and preferably, respectively, between 0.001 and 10% by weight of mequinol relative to the total weight of the composition and between 0.05 and 10% by weight of depigmenting agent relative to the total weight of the composition. The composition can also comprise at least one sunscreen in preferential concentrations ranging from 0.001 to 30.00% by weight relative to the total weight of the composition. Among the sun filters, non-limiting examples that may be mentioned include physical sun filters such as titanium dioxide, zinc oxide and chemical sun filters such as octocrylene, ethylhexyl methoxycinnamate, octyl salicylate, avobenzone, oxybenzone, ecamsule or drometrizole trisiloxane, or mixtures thereof.
Dans une variante de réalisation de la présente invention, la composition pourra comprendre plusieurs filtres solaires. Auquel cas, chaque filtre solaire pourra être ajouté à une concentration allant de 0.001 à 20% en poids par rapport au poids total de la composition.In an alternative embodiment of the present invention, the composition may include several sun filters. In which case, each sunscreen can be added at a concentration ranging from 0.001 to 20% by weight relative to the total weight of the composition.
Les compositions selon l'invention peuvent comprendre en outre tout additif usuellement utilisé dans le domaine cosmétique ou pharmaceutique, tel que des séquestrants, des antioxydants, des conservateurs, des charges, des électrolytes, des humectants, des colorants, de bases ou d'acides usuels, minéraux ou organiques, des parfums, des huiles essentielles, des actifs cosmétiques, des hydratants, des vitamines, des acides gras essentiels, des sphingolipides, des composés autobronzants, des agents apaisants et protecteurs de la peau. Bien entendu l'homme du métier veillera à choisir ce ou ces éventuels composés complémentaires, et/ou leur quantité, de manière telle que les propriétés avantageuses de la composition selon l'invention ne soient pas, ou substantiellement pas, altérées.The compositions according to the invention may also comprise any additive usually used in the cosmetic or pharmaceutical field, such as sequestrants, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids usual, mineral or organic, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, soothing and protective agents for the skin. Of course, a person skilled in the art will take care to choose this or these optional additional compounds, and / or their quantity, in such a way that the advantageous properties of the composition according to the invention are not, or not substantially, altered.
Ces additifs peuvent être présents dans la composition à raison de 0,001 à 20 % en poids par rapport au poids total de la composition.These additives can be present in the composition in an amount of 0.001 to 20% by weight relative to the total weight of the composition.
La présente invention a aussi pour objet une composition pharmaceutique telle que décrite précédemment à titre de médicament.The present invention also relates to a pharmaceutical composition as described above as a medicament.
La présente invention a également pour objet une composition cosmétique.The present invention also relates to a cosmetic composition.
Les compositions contenant l'association selon l'invention peuvent présenter toutes les formes galeniques normalement utilisées pour une application topique, par exemple sous forme de solutions, de gels, de dispersions du type lotion ou sérum, d'émulsions de consistance liquide ou semi-liquide du type lait, obtenues par dispersion d'une phase grasse dans une phase aqueuse (H/E) ou inversement (E/H), ou de suspensions ou émulsions de consistance molle, semi-solide ou solide du type crème ou gel, ou encore de microémulsions, de microcapsules, de microparticules ou de dispersions vésiculaires de type ionique et/ou non ionique. Ces compositions sont préparées selon les méthodes usuelles.The compositions containing the combination according to the invention can have all the dosage forms normally used for topical application, for example in the form of solutions, gels, dispersions of the lotion or serum type, emulsions of liquid or semi-liquid consistency of the milk type, obtained by dispersion of a fatty phase in an aqueous phase (O / W) or vice versa (W / O), or of suspensions or emulsions of soft, semi-solid or solid consistency of cream or gel type, or else microemulsions, microcapsules, microparticles or vesicular dispersions of ionic and / or nonionic type. These compositions are prepared according to the usual methods.
De façon connue, les compositions cosmétiques ou dermatologiques de l'invention peuvent contenir des adjuvants habituels dans le domaine cosmétique ou dermatologique, tels que les emulsionnants, les gélifiants hydrophiles ou lipophiles, les actifs hydrophiles ou lipophiles différents de l'oxyde de titane et de l'α-hydroxyacide, les conservateurs, les antioxydants, les parfums, les charges, les filtres et les matières colorantes. Les quantités de ces différents adjuvants sont celles classiquement utilisées dans les domaines cosmétique et/ou dermatologique, et par exemple de 0,01 % à 20 % du poids total de la composition. Ces adjuvants, selon leur nature, peuvent être introduits dans la phase grasse, dans la phase aqueuse et/ou dans les vésicules lipidiques.In known manner, the cosmetic or dermatological compositions of the invention may contain adjuvants customary in the cosmetic or dermatological field, such as emulsifiers, hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents other than titanium oxide and α-hydroxy acid, preservatives, antioxidants, perfumes, fillers, filters and coloring matters. The amounts of these various adjuvants are those conventionally used in the cosmetic and / or dermatological fields, and for example from 0.01% to 20% of the total weight of the composition. These adjuvants, depending on their nature, can be introduced into the fatty phase, into the aqueous phase and / or into the lipid vesicles.
L'invention se rapporte également à l'utilisation de la composition selon l'invention telle que décrite précédemment dans le domaine pharmaceutique et cosmétique.The invention also relates to the use of the composition according to the invention as described above in the pharmaceutical and cosmetic field.
Les compositions de l'invention conviennent particulièrement bien au traitement et à la prévention des désordres de la pigmentation. Préférentiellement, les compositions de l'invention conviennent au traitement et à la prévention des désordres hyperpigmentaires tels que le melasma, le chloasma, les lentigines, le lentigo sénile, le vitiligo, les taches de rousseur, les hyperpigmentations post-inflammatoires dues à une abrasion, une brûlure, une cicatrice, une dermatose, une allergie de contact; les nevi, les hyperpigmentations à déterminisme génétique, les hyperpigmentations d'origine métabolique ou médicamenteuse, les mélanomes ou toutes autres lésions hyperpigmentaires notamment celles induites par le vieillissement photo induit ou chronologique de la peau et des phanères.The compositions of the invention are particularly suitable for the treatment and prevention of pigmentation disorders. Preferably, the compositions of the invention are suitable for the treatment and prevention of hyperpigmentary disorders such as melasma, chloasma, lentigines, senile lentigo, vitiligo, freckles, post-inflammatory hyperpigmentations due to abrasion. , a burn, a scar, a dermatosis, a contact allergy; nevi, hyperpigmentations with genetic determinism, hyperpigmentations of metabolic or drug origin, melanomas or any other hyperpigmentary lesions in particular those induced by photo induced or chronological aging of the skin and integuments.
Plus préférentiellement les compositions selon l'invention conviennent au traitement du mélasma. Les compositions selon l'invention trouvent également une application dans le domaine cosmétique, en particulier dans la protection contre les aspects néfastes du soleil, en particulier contre les taches pigmentaires.More preferably, the compositions according to the invention are suitable for the treatment of melasma. The compositions according to the invention also find an application in the cosmetic field, in particular in protection against the harmful aspects of the sun, in particular against pigmentary spots.
L'invention porte également sur un procédé de traitement cosmétique non thérapeutique d'embellissement de la peau et/ou d'amélioration de son aspect de surface, caractérisé par le fait que l'on applique sur la peau et/ou ses phanères une composition comprenant du mequinol et au moins un agent dépigmentant.The invention also relates to a non-therapeutic cosmetic treatment process for beautifying the skin and / or improving its surface appearance, characterized in that a composition is applied to the skin and / or its integuments comprising mequinol and at least one depigmenting agent.
Les exemples de formulations ci-dessous permettent d'illustrer les compositions selon l'invention, sans toutefois en limiter la portée. Des exemples illustrant l'activité dépigmentante des différentes compositions selon l'invention, sont également décrits.The examples of formulations below make it possible to illustrate the compositions according to the invention, without however limiting their scope. Examples illustrating the depigmenting activity of the various compositions according to the invention are also described.
Dans les compositions ci-après (exemples 1 à 6), les proportions des différents constituants sont exprimées en pourcentage en poids par rapport au poids total de la composition.In the compositions below (examples 1 to 6), the proportions of the various constituents are expressed as a percentage by weight relative to the total weight of the composition.
Exemple 1 :Example 1:
Figure imgf000006_0001
Exemple 2 :
Figure imgf000006_0001
Example 2:
Figure imgf000007_0001
Figure imgf000007_0001
Exemple 3Example 3
Figure imgf000007_0002
Figure imgf000007_0002
Exemple 4 :Example 4:
Figure imgf000007_0003
Figure imgf000007_0003
Figure imgf000008_0001
Figure imgf000008_0001
Exemple 5 :Example 5:
Figure imgf000008_0002
Figure imgf000008_0002

Claims

Revendications claims
1. Composition dépigmentante de la peau comprenant, dans un véhicule physiologiquement acceptable, du mequinol et au moins un agent dépigmentant choisi dans la liste constituée par l'acide kojique et ses dérivés ; l'acide azélaique et ses dérivés ; les acides dicarboxyliques ; la vitamine C et ses dérivés, l'arbutine et ses dérivés et le paracetamol.1. Skin depigmenting composition comprising, in a physiologically acceptable vehicle, mequinol and at least one depigmenting agent chosen from the list consisting of kojic acid and its derivatives; azelaic acid and its derivatives; dicarboxylic acids; vitamin C and its derivatives, arbutin and its derivatives and paracetamol.
2. Composition selon la revendication 1 , caractérisée en ce que l'agent dépigmentant est l'arbutine, le paracetamol ou la vitamine C.2. Composition according to claim 1, characterized in that the depigmenting agent is arbutin, paracetamol or vitamin C.
3. Composition selon l'une quelconque des revendications de 1 à 2, caractérisée en ce qu'elle contient également au moins un filtre solaire.3. Composition according to any one of claims 1 to 2, characterized in that it also contains at least one sunscreen.
4. Composition selon l'une quelconque des revendications de 1 à 3 à titre de médicament.4. Composition according to any one of claims 1 to 3 as a medicament.
5. Composition selon d'une quelconque des revendications 1 à 3 caractérisé en ce que la composition est une composition cosmétique.5. Composition according to any one of claims 1 to 3 characterized in that the composition is a cosmetic composition.
Utilisation d'une composition dépigmentante de la peau, comprenant du mequinol et au moins un agent dépigmentant dans un véhicule physiologiquement acceptable pour la fabrication d'une préparation pharmaceutique destinée à prévenir ou à traiter des désordres de la pigmentation.Use of a depigmenting composition for the skin, comprising mequinol and at least one depigmenting agent in a physiologically acceptable vehicle for the manufacture of a pharmaceutical preparation intended for preventing or treating pigmentation disorders.
Utilisation d'une composition selon la revendication 6 pour la fabrication d'une préparation pharmaceutique destinée à prévenir ou à traiter le melasma.Use of a composition according to claim 6 for the manufacture of a pharmaceutical preparation intended for preventing or treating melasma.
8. Utilisation cosmétique d'une composition dépigmentante de la peau, comprenant du mequinol et au moins un agent dépigmentant dans un véhicule physiologiquement acceptable, pour la protection contre les aspects néfastes du soleil.8. Cosmetic use of a depigmenting composition for the skin, comprising mequinol and at least one depigmenting agent in a physiologically acceptable vehicle, for protection against the harmful aspects of the sun.
9. utilisation cosmétique d'une composition dépigmentante de la peau, comprenant du mequinol et au moins un agent dépigmentant dans un véhicule physiologiquement acceptable comme agent de blanchiment de la peau. 9. cosmetic use of a skin depigmenting composition, comprising mequinol and at least one depigmenting agent in a physiologically acceptable vehicle as skin whitening agent.
0. Procédé de traitement cosmétique non thérapeutique d'embellissement de la peau et/ou d'amélioration de son aspect de surface, caractérisé par le fait que l'on applique sur la peau et/ou ses phanères une composition comprenant du mequinol et au moins un agent dépigmentant. 0. A non-therapeutic cosmetic treatment process for beautifying the skin and / or improving its surface appearance, characterized in that a composition comprising mequinol and at least one is applied to the skin and / or its integuments. minus a depigmenting agent.
PCT/FR2005/001211 2004-05-14 2005-05-13 Pharmaceutical or cosmetic composition comprising mequinol and at least one depigmenting agent WO2005115365A2 (en)

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CA002564104A CA2564104A1 (en) 2004-05-14 2005-05-13 Pharmaceutical or cosmetic composition comprising mequinol and at least one depigmenting agent
US11/596,356 US20080159969A1 (en) 2004-05-14 2005-05-13 Pharmaceutical Or Cosmetic Composition Comprising Mequinol And At Least One Depigmenting Agent

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